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(R)-GNE-140 - 98%, high purity , CAS No.2003234-63-5

COA COA
    Grade & Purity:
  • ≥98%
In stock
Item Number
R413580
Grouped product items
SKU Size
Availability
 Price Qty
R413580-1mg
1mg
3
$59.90
R413580-5mg
5mg
3
$159.90
R413580-10mg
10mg
2
$269.90
R413580-25mg
25mg
2
$509.90
R413580-50mg
50mg
2
$719.90
R413580-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$999.90
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Bulk Order  SDS  DATASHEET  Specification Sheet

Dehydrogenase Inhibitors

View related series
Glucose Metabolism (1943) Lactate Dehydrogenase (31) Metabolic Enzyme/Protease (4860)

Basic Description

Synonyms 2(1H)-Pyridinone,3-[(2-chlorophenyl)thio]-5,6-dihydro-4-hydroxy-6-[4-(4-morpholinyl)phenyl]-6-(3-thienyl)-,(6R)-
Specifications & Purity ≥98%
Biochemical and Physiological Mechanisms (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Information

(R)-GNE-140 (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.


Targets

LDHA (Cell-free assay); LDHB (Cell-free assay) 3 nM; 5 nM


In vitro

(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 μM. (R)-GNE-140 exhibits inhibition with two chondrosarcoma (bone) cancer cell lines that harbored IDH1 mutations (IC50 = 0.8μM).(R)-GNE-140 has submicromolar MiaPaca2 potency and inhibits proliferation in 11% of cancer cell lines in a broad panel.


In vivo

(R)-GNE-140 presents a low Clp, and also had high bioavailability when dosed orally at 5 mg/kg to mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater in vivo exposure.


Cell Research(from reference)

Cell lines：105KC,JJ012,143B,G84,1321N1,ONS-76,G22,G140,G96,HCC1143,CAL-120,Hs 578T,SISO,SKG-II,HCT-15,KYSE-520,KMRC-1,SNU-475,SNU-423,HT-1080,NCI-H1437,NCI-H1339,LXF-289,MCAS,PA-1,Hs 38.T,59M,MIA PaCa-2,SW 1990,PSN1,GR-M,Hs 746T,MKN-74,S-117,FTC-238,B-CP 

Concentrations：6 pt dose titration scheme 

Incubation Time：72 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Oxazinanes
Subclass Morpholines
Intermediate Tree Nodes Not available
Direct Parent Phenylmorpholines
Alternative Parents Dialkylarylamines  Aryl thioethers  Aniline and substituted anilines  Dihydropyridines  Chlorobenzenes  Aryl chlorides  Thiophenes  Heteroaromatic compounds  Cyclic carboximidic acids  Thioenol ethers  Sulfenyl compounds  Propargyl-type 1,3-dipolar organic compounds  Oxacyclic compounds  Dialkyl ethers  Azacyclic compounds  Organopnictogen compounds  Organochlorides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Phenylmorpholine - Aryl thioether - Aniline or substituted anilines - Dialkylarylamine - Tertiary aliphatic/aromatic amine - Halobenzene - Dihydropyridine - Chlorobenzene - Benzenoid - Hydropyridine - Monocyclic benzene moiety - Aryl halide - Aryl chloride - Heteroaromatic compound - Cyclic carboximidic acid - Thiophene - Thioenolether - Tertiary amine - Oxacycle - Azacycle - Organic 1,3-dipolar compound - Propargyl-type 1,3-dipolar organic compound - Sulfenyl compound - Ether - Dialkyl ether - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Hydrocarbon derivative - Organosulfur compound - Organooxygen compound - Organonitrogen compound - Organochloride - Organohalogen compound - Amine - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylmorpholines. These are aromatic compounds containing a morpholine ring and a benzene ring linked to each other through a CC or a CN bond.
External Descriptors Not available

Associated Targets(Human)

LDHB Tchem L-lactate dehydrogenase B chain (2 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LDHA Tchem L-lactate dehydrogenase A chain (6 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LDHA Tchem L-lactate dehydrogenase A chain (1573 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LDHB Tchem L-lactate dehydrogenase B chain (463 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A673 (619 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MCF7 (126967 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MG-63 (795 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NCI-H1975 (4994 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A549 (127892 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MIA PaCa-2 (5949 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IDH1 Tclin Isocitrate dehydrogenase [NADP] cytoplasmic (40980 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEL-S-133P L-lactate dehydrogenase (161 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BEAS-2B (690 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name (2R)-5-(2-chlorophenyl)sulfanyl-4-hydroxy-2-(4-morpholin-4-ylphenyl)-2-thiophen-3-yl-1,3-dihydropyridin-6-one
INCHI InChI=1S/C25H23ClN2O3S2/c26-20-3-1-2-4-22(20)33-23-21(29)15-25(27-24(23)30,18-9-14-32-16-18)17-5-7-19(8-6-17)28-10-12-31-13-11-28/h1-9,14,16,29H,10-13,15H2,(H,27,30)/t25-/m1/s1
InChIKey SUFXXEIVBZJOAP-RUZDIDTESA-N
Smiles C1COCCN1C2=CC=C(C=C2)C3(CC(=C(C(=O)N3)SC4=CC=CC=C4Cl)O)C5=CSC=C5
Isomeric SMILES C1COCCN1C2=CC=C(C=C2)[C@]3(CC(=C(C(=O)N3)SC4=CC=CC=C4Cl)O)C5=CSC=C5
PubChem CID 121225870
Molecular Weight 499.04

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

7 results found

Lot Number Certificate Type Date Item
A2408629 Certificate of Analysis Dec 07, 2023 R413580
A2408636 Certificate of Analysis Dec 07, 2023 R413580
A2408638 Certificate of Analysis Dec 07, 2023 R413580
A2408639 Certificate of Analysis Dec 07, 2023 R413580
A2408640 Certificate of Analysis Dec 07, 2023 R413580
A2408641 Certificate of Analysis Dec 07, 2023 R413580
A2408637 Certificate of Analysis Dec 07, 2023 R413580

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 30 mg/mL (60.11 mM); Water: Insoluble; Ethanol: Insoluble;
Molecular Weight 499.000 g/mol
XLogP3 4.800
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 5
Exact Mass 498.084 Da
Monoisotopic Mass 498.084 Da
Topological Polar Surface Area 115.000 Ų
Heavy Atom Count 33
Formal Charge 0
Complexity 739.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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